2010 Vol. 28, No. 2
Display Method:
2010, 28(2): 94-96,111.
Abstract:
About half of the drugs in use are chiral,however,that in most cases the pharmacological activity is restricted to one of the enantiomers(eutomer) whereas the other enantiomer(distomer) can be even toxic.The development of Methods for enantioselective analysis became very important for drug quality control.Cyclodextrins(CDs) are the most frequently used chiral selectors in chiral separation and analysis.In this paper,the recently application of cyclodextrin and its derivatives were reviewed,which involved HPLC,GC,CE,MS and SFC.
About half of the drugs in use are chiral,however,that in most cases the pharmacological activity is restricted to one of the enantiomers(eutomer) whereas the other enantiomer(distomer) can be even toxic.The development of Methods for enantioselective analysis became very important for drug quality control.Cyclodextrins(CDs) are the most frequently used chiral selectors in chiral separation and analysis.In this paper,the recently application of cyclodextrin and its derivatives were reviewed,which involved HPLC,GC,CE,MS and SFC.
2010, 28(2): 101-104.
Abstract:
Objective The antibiotic tests of different polar extracts of Artemisia anomala S.Moore in vitro. Methods The antibiotic tests of different polar extracts of AASM in vitro were performed by using Kirby-Bauer method and broth dilution method. Results The minimal bactericidal concentration(MBC) of 80% ethyl alcohol extract of Artemisia anomala S.Moore is 25 mg/ml for Shigella dysenteriae.The MBC of chloroform extract is 6.25 mg/ml for Escherichia coli.The MBC of chloroform extract is 12.5 mg/ml for staphylococcus aureus.The MBC of acetic ether extract is 6.25 mg/ml for Shigella flexneri,Shigella dysenteriae and Streptococcus agalactiae.The MBC of acetic ether extract is 12.5 mg/ml for staphylococcus aureus.The MBC of butanol extract of is 12.5 mg/ml for Streptococcus agalactiae.The MBC of butanol extract is 25 mg/ml for Shigella dysenteriae.Petroleum ether extract did not show significant antibacterial activity. Conclusion Different polar parts of Artemisia anomala S.Moore on a variety of clinical pathogenic bacteria showed good bactericidal effect in vitro.Thus,at the anti-infective therapeutic areas there are great prospects for development and application.The effective monomer of Artemisia anomala and its bactericidal mechanism needs further study.
Objective The antibiotic tests of different polar extracts of Artemisia anomala S.Moore in vitro. Methods The antibiotic tests of different polar extracts of AASM in vitro were performed by using Kirby-Bauer method and broth dilution method. Results The minimal bactericidal concentration(MBC) of 80% ethyl alcohol extract of Artemisia anomala S.Moore is 25 mg/ml for Shigella dysenteriae.The MBC of chloroform extract is 6.25 mg/ml for Escherichia coli.The MBC of chloroform extract is 12.5 mg/ml for staphylococcus aureus.The MBC of acetic ether extract is 6.25 mg/ml for Shigella flexneri,Shigella dysenteriae and Streptococcus agalactiae.The MBC of acetic ether extract is 12.5 mg/ml for staphylococcus aureus.The MBC of butanol extract of is 12.5 mg/ml for Streptococcus agalactiae.The MBC of butanol extract is 25 mg/ml for Shigella dysenteriae.Petroleum ether extract did not show significant antibacterial activity. Conclusion Different polar parts of Artemisia anomala S.Moore on a variety of clinical pathogenic bacteria showed good bactericidal effect in vitro.Thus,at the anti-infective therapeutic areas there are great prospects for development and application.The effective monomer of Artemisia anomala and its bactericidal mechanism needs further study.
2010, 28(2): 105-106,121.
Abstract:
Objective To identify the composition of the total alkaloids of the seeds of Caragana microphylla,a native plant from the North west of China which is used in traditional Mongolian medicines. Methods The alkaloids was separated and identified by chromatographic Methods and spectral analysis.The anticancer activities of the total alkaloids and the isolated protoberberine alkaloids were tested respectively on Saos-2,A375 and Hela cell lines. Results Five protoberberine alkaloids including dehydrothalictrifoline,coptisine,epiberberine,dehydroapocavidine and corysamine were isolated.The totel alkaloids and the 5 alkaloids were found to be very effective against three tumor cell lines. Conclusion s The 5 protoberberine alkaloids were isolated for the first time from Caragana genus.Caragana microphylla seed extracts may play a role as an hopefulanticancer therapeutic agent.
Objective To identify the composition of the total alkaloids of the seeds of Caragana microphylla,a native plant from the North west of China which is used in traditional Mongolian medicines. Methods The alkaloids was separated and identified by chromatographic Methods and spectral analysis.The anticancer activities of the total alkaloids and the isolated protoberberine alkaloids were tested respectively on Saos-2,A375 and Hela cell lines. Results Five protoberberine alkaloids including dehydrothalictrifoline,coptisine,epiberberine,dehydroapocavidine and corysamine were isolated.The totel alkaloids and the 5 alkaloids were found to be very effective against three tumor cell lines. Conclusion s The 5 protoberberine alkaloids were isolated for the first time from Caragana genus.Caragana microphylla seed extracts may play a role as an hopefulanticancer therapeutic agent.
2010, 28(2): 107-111.
Abstract:
Objective To study the inhibition of mimic peptides binding specifically with the first and second extra-cellular domain of the CC chemokine receptor 5(CCR5) on mice ear engorgement induced by dimethyl benzene. Methods Phage display peptide library was used to screen peptide sequence bonding specifically with CCR5,then the model of mice ear engorgement was establish,and the four mimic peptides whose amino acid sequence are respectively STFTTTL(SL)、TPITQLL(TL)、SLPLPKP(SP)、QTSSAAL(QL) was synthesized,and the four peptides was injected into abdominal cavity of the ear engorgement model mice,take aspirin as the positive control of anti-inflammatory pharmacodynamics experiment.The left and the right mice ear tissue were obtained and weighted、HE stained,the four peptides was investigated the anti-inflammatory activity to mice ear engorgement induced by dimethyl benzene. Results After the left and the right mice ear tissue were weighted and HE stained,we find the four CCR5 mimic peptides had suppressed significantly mice ear engorgement induced by dimethyl benzene、hydrops and infiltrating of the inflammatory cells.The inhibition ratio is respectively 53.4%、47.3%、31.3%、25.2% that effect is significant(P<0.05). Conclusion All of the four short peptides respectively take the evident suppressing role on mice ear engorgement induced by dimethyl benzene.Thus this study indicated CCR5 may play a important role in the course of mice ear engorgement induced by dimethyl benzene.
Objective To study the inhibition of mimic peptides binding specifically with the first and second extra-cellular domain of the CC chemokine receptor 5(CCR5) on mice ear engorgement induced by dimethyl benzene. Methods Phage display peptide library was used to screen peptide sequence bonding specifically with CCR5,then the model of mice ear engorgement was establish,and the four mimic peptides whose amino acid sequence are respectively STFTTTL(SL)、TPITQLL(TL)、SLPLPKP(SP)、QTSSAAL(QL) was synthesized,and the four peptides was injected into abdominal cavity of the ear engorgement model mice,take aspirin as the positive control of anti-inflammatory pharmacodynamics experiment.The left and the right mice ear tissue were obtained and weighted、HE stained,the four peptides was investigated the anti-inflammatory activity to mice ear engorgement induced by dimethyl benzene. Results After the left and the right mice ear tissue were weighted and HE stained,we find the four CCR5 mimic peptides had suppressed significantly mice ear engorgement induced by dimethyl benzene、hydrops and infiltrating of the inflammatory cells.The inhibition ratio is respectively 53.4%、47.3%、31.3%、25.2% that effect is significant(P<0.05). Conclusion All of the four short peptides respectively take the evident suppressing role on mice ear engorgement induced by dimethyl benzene.Thus this study indicated CCR5 may play a important role in the course of mice ear engorgement induced by dimethyl benzene.
2010, 28(2): 112-113,125.
Abstract:
Objective To observe the effects of tentacle-only extract(TOE) from Cyanea capillata on the conduction system of isolated rat heart and investigate the mechanism of its cardiac toxicity. Methods Seventy-two Sprague Dawley(SD) rats were randomly divided into six groups(n=12),and Langendorff heart perfusion models were established,then different doses of TOE were applied to each group to observe the effects of TOE on the conduction system of the isolated rat hearts. Results Compared with the control group,all the doses of TOE induced a significant decrease of heart rate,and the incidence of arrhythmia was significantly increased.Moreover,both the effects were dose-dependent. Conclusion The TOE of C.capillata induced significant changes of the conduction system of isolated rat heart,which could partly interpret the mechanism of its cardiac toxicity.
Objective To observe the effects of tentacle-only extract(TOE) from Cyanea capillata on the conduction system of isolated rat heart and investigate the mechanism of its cardiac toxicity. Methods Seventy-two Sprague Dawley(SD) rats were randomly divided into six groups(n=12),and Langendorff heart perfusion models were established,then different doses of TOE were applied to each group to observe the effects of TOE on the conduction system of the isolated rat hearts. Results Compared with the control group,all the doses of TOE induced a significant decrease of heart rate,and the incidence of arrhythmia was significantly increased.Moreover,both the effects were dose-dependent. Conclusion The TOE of C.capillata induced significant changes of the conduction system of isolated rat heart,which could partly interpret the mechanism of its cardiac toxicity.
2010, 28(2): 114-115,153.
Abstract:
Objective To investigate the technology of total flavonoids in Sedum sarmentosum extracted by enzymatic method and its antibacterial activity. Methods Total flavonoids in Sedum sarmentosum was extracted by the method that enzymatic hydrolysis combined with water decocting.The extraction technology was optimized by orthogonal design with the content of total flavonoids yield.The antibacterial activity of total flavonoids was determined by stiletto method.The Results reveled that the optimum technology was to be hydrolyzed for 1.5 h by 0.6% enzyme at 50 ℃ in pH 6.0.The significant factor was the temperature of enzymatic hydrolysis.The yield of total flavonoids was 3.471%.Total flavonoids of Sedum sarmentosum was bacteriostasis on E.coli,Staphylococcus aureus,Bacillus subtilis and Bacillus gasoformans.The bacteriostasis on Bacillus aerogenes was not obvious.The extraction technology obtained in this experiment are reasonable and feasible with high extraction rate,and the total flavonoids has some antibacterial activity.
Objective To investigate the technology of total flavonoids in Sedum sarmentosum extracted by enzymatic method and its antibacterial activity. Methods Total flavonoids in Sedum sarmentosum was extracted by the method that enzymatic hydrolysis combined with water decocting.The extraction technology was optimized by orthogonal design with the content of total flavonoids yield.The antibacterial activity of total flavonoids was determined by stiletto method.The Results reveled that the optimum technology was to be hydrolyzed for 1.5 h by 0.6% enzyme at 50 ℃ in pH 6.0.The significant factor was the temperature of enzymatic hydrolysis.The yield of total flavonoids was 3.471%.Total flavonoids of Sedum sarmentosum was bacteriostasis on E.coli,Staphylococcus aureus,Bacillus subtilis and Bacillus gasoformans.The bacteriostasis on Bacillus aerogenes was not obvious.The extraction technology obtained in this experiment are reasonable and feasible with high extraction rate,and the total flavonoids has some antibacterial activity.
2010, 28(2): 116-117,133.
Abstract:
Objective To optimize the extraction technology for Sanhuang Jiedu cream. Methods The optimum extraction technology for Sanhuang Jiedu cream was investigated by the L9(34) orthogonal test with the total amount of the dry extract and the content of berberine hydrochloride as technology index.The influence factors including the concentration of ethanol,solvent ratio,extraction times,time length of extraction. Results The optimum extraction technology was: the solid-liquid ratio was 110;the concentration of ethanol was 70%;the refluxing extraction was carried out for 3 times(1hours/time). Conclusion The optimum extraction technology for Sanhuang Jiedu cream is stable and feasible.
Objective To optimize the extraction technology for Sanhuang Jiedu cream. Methods The optimum extraction technology for Sanhuang Jiedu cream was investigated by the L9(34) orthogonal test with the total amount of the dry extract and the content of berberine hydrochloride as technology index.The influence factors including the concentration of ethanol,solvent ratio,extraction times,time length of extraction. Results The optimum extraction technology was: the solid-liquid ratio was 110;the concentration of ethanol was 70%;the refluxing extraction was carried out for 3 times(1hours/time). Conclusion The optimum extraction technology for Sanhuang Jiedu cream is stable and feasible.
2010, 28(2): 118-121.
Abstract:
Objective To preparation of ginkgo biloba leaf in-situ nasal gel and exploration of the effect of sorbefacients on nasal mucosa Absorption. Methods Carbopol 934 and HPMC were used as gel matrix to prepare pH sensitive in-situ ginkgo biloba leaf nasal gel,whose viscosity,adhesion,and in vitro nasal mucosa Absorption were studied. Results The in-situ ginkgo biloba leaf gel can be best prepared with 0.8% of Carbopol 934 and 1.5% of HPMC as gel matrix.Three sorbefacients were studied.The sequence of their permeation rate were 1% of Azone > 1% of Twain-80 > 0.5% of Borneol.The drug Absorption rate increases as the Azone concentration increases,the it’s Absorption process fits Weibull equation. Conclusion The preparation technology of in-situ ginkgo biloba leaf nasal gel is viable.And Azone is the most effective sorbefacient for nasal mucosa Absorption.
Objective To preparation of ginkgo biloba leaf in-situ nasal gel and exploration of the effect of sorbefacients on nasal mucosa Absorption. Methods Carbopol 934 and HPMC were used as gel matrix to prepare pH sensitive in-situ ginkgo biloba leaf nasal gel,whose viscosity,adhesion,and in vitro nasal mucosa Absorption were studied. Results The in-situ ginkgo biloba leaf gel can be best prepared with 0.8% of Carbopol 934 and 1.5% of HPMC as gel matrix.Three sorbefacients were studied.The sequence of their permeation rate were 1% of Azone > 1% of Twain-80 > 0.5% of Borneol.The drug Absorption rate increases as the Azone concentration increases,the it’s Absorption process fits Weibull equation. Conclusion The preparation technology of in-situ ginkgo biloba leaf nasal gel is viable.And Azone is the most effective sorbefacient for nasal mucosa Absorption.
2010, 28(2): 122-125.
Abstract:
Objective To develop the pH-triggered levofloxacin hydrochloride in-situ forming eye gel. Methods The gel was formed carpool as gel base and hydroxypropyl methylcellulose(HPMC) as thickening agents,and was the foluma evaluated according to the viscosity,the in-situ gelling capacity and the content of levofloxacin hydrochloride. Results The optimized formulation was made by dissolving levofloxacin hydrochloride 0.1 g,HPMC E50LV 2.0 g,carbopol 0.3 g,Na2HPO4 0.35 g,NaH2PO4 0.45 g,NaCl 0.50 g,and ethylparaben 0.03 g in 100 ml water.The gels showed good sustained release characteristics in vitro. Conclusion The optimized formulation has a good reproducibility and can be used for preparation of pH-triggered levofloxacin hydrochloride in-situ forming eye gel.
Objective To develop the pH-triggered levofloxacin hydrochloride in-situ forming eye gel. Methods The gel was formed carpool as gel base and hydroxypropyl methylcellulose(HPMC) as thickening agents,and was the foluma evaluated according to the viscosity,the in-situ gelling capacity and the content of levofloxacin hydrochloride. Results The optimized formulation was made by dissolving levofloxacin hydrochloride 0.1 g,HPMC E50LV 2.0 g,carbopol 0.3 g,Na2HPO4 0.35 g,NaH2PO4 0.45 g,NaCl 0.50 g,and ethylparaben 0.03 g in 100 ml water.The gels showed good sustained release characteristics in vitro. Conclusion The optimized formulation has a good reproducibility and can be used for preparation of pH-triggered levofloxacin hydrochloride in-situ forming eye gel.
Preparation of sirolimus sustained-release tables and observe of influence factors on releasing drug
2010, 28(2): 126-129,139.
Abstract:
Objective To prepare the sirolimus sustained-release tablets and study the influence factor. Methods The sirolimus sustained-release tablets were prepared by HPMC as the matrix material.The effects of viscosity of HPMC,sort of an adhensive amount of a lubricant,and the preparation Methods on the release of sirolimus from matrix tablets were observed. Results Based on the Results of single factor tests,an optimal self-prepared matrix sustsained-release tablets which contained 30 % HPMC(K4M),2 % lactose and MCC was definited.The release of the drug was an obvious characteristic in first class. Conclusion The tables have desirable sustain-release property in vitro.The preparation process was simple and can be applied in production.
Objective To prepare the sirolimus sustained-release tablets and study the influence factor. Methods The sirolimus sustained-release tablets were prepared by HPMC as the matrix material.The effects of viscosity of HPMC,sort of an adhensive amount of a lubricant,and the preparation Methods on the release of sirolimus from matrix tablets were observed. Results Based on the Results of single factor tests,an optimal self-prepared matrix sustsained-release tablets which contained 30 % HPMC(K4M),2 % lactose and MCC was definited.The release of the drug was an obvious characteristic in first class. Conclusion The tables have desirable sustain-release property in vitro.The preparation process was simple and can be applied in production.
2010, 28(2): 130-133.
Abstract:
The selection method of separation condition and cyclodextrin and strategy of chiral separation by capillary electrophoresis were summarized,and a general research and development strategy was proposed,which can provide basis for chiral separation by capillary electrophoresis.
The selection method of separation condition and cyclodextrin and strategy of chiral separation by capillary electrophoresis were summarized,and a general research and development strategy was proposed,which can provide basis for chiral separation by capillary electrophoresis.
2010, 28(2): 134-136.
Abstract:
Objective To establish a method for determination of uracil and auantion in Eupolyphaga seu Steleophaga by HPLC. Methods The HPLC separation was performed on Alltima NH2(150 mm×4.6 mm,5 μm)column with a mixture of acetonitrile-water(9010)as the mobile phase,at a flow rate of 1.0 ml/min.Detection wavelength was at 205 nm,and column temperature was at 35 ℃. Results The linear response of Auantion and Uracil range from 0.404～3.23 μg(r=0.999 5,n=5)and 0.820～6.56 μg(r=0.999 5,n=5);the average recovery was 98.8% with RSD 0.96% and 99.0% with RSD 0.79% respectively(n=6). Conclusion The method is simple,accurate and suitable for the determination of auantion and uracil in Eupolyphaga seu Steleophaga.
Objective To establish a method for determination of uracil and auantion in Eupolyphaga seu Steleophaga by HPLC. Methods The HPLC separation was performed on Alltima NH2(150 mm×4.6 mm,5 μm)column with a mixture of acetonitrile-water(9010)as the mobile phase,at a flow rate of 1.0 ml/min.Detection wavelength was at 205 nm,and column temperature was at 35 ℃. Results The linear response of Auantion and Uracil range from 0.404～3.23 μg(r=0.999 5,n=5)and 0.820～6.56 μg(r=0.999 5,n=5);the average recovery was 98.8% with RSD 0.96% and 99.0% with RSD 0.79% respectively(n=6). Conclusion The method is simple,accurate and suitable for the determination of auantion and uracil in Eupolyphaga seu Steleophaga.
2010, 28(2): 137-139.
Abstract:
Objective To establish an effective quality control method of the traditional Chinese medicine——Polygala japonica Houtt. Methods HPLC-ELSD method was adopted for the determination of polygalasaponin F in Polygala japonica Houtt.The analysis was performed on a SHISEIDO Capcell Pak C18(4.6 mm×250 mm,5 μm) as the analytical column,acetonitrile-water(3070,v/v) as the mobile phase.The flow rate was 1.0 ml/min.The column temperature was at 25 ℃. Results The validation was carried out and the linearity(r2 = 0.999 8) between 0.346 μg and 3.460 μg and recovery(99.85%) were acceptable.The precision and reproducibility were evaluated with RSD values 1.64% and 2.12%,respectively. Conclusion This method is simple and feasible for the determination of polygalasaponin F in Polygala japonica Houtt.
Objective To establish an effective quality control method of the traditional Chinese medicine——Polygala japonica Houtt. Methods HPLC-ELSD method was adopted for the determination of polygalasaponin F in Polygala japonica Houtt.The analysis was performed on a SHISEIDO Capcell Pak C18(4.6 mm×250 mm,5 μm) as the analytical column,acetonitrile-water(3070,v/v) as the mobile phase.The flow rate was 1.0 ml/min.The column temperature was at 25 ℃. Results The validation was carried out and the linearity(r2 = 0.999 8) between 0.346 μg and 3.460 μg and recovery(99.85%) were acceptable.The precision and reproducibility were evaluated with RSD values 1.64% and 2.12%,respectively. Conclusion This method is simple and feasible for the determination of polygalasaponin F in Polygala japonica Houtt.
2010, 28(2): 140-142.
Abstract:
Objective To conclude the Practice and experience of prescription evaluation program. Methods To take a sample of 120 prescriptions every month during July 2007 to July 2009,calculate the average of each indicator of the prescription evaluation table designed by the Ministry of Health. Results average numbers of drugs per prescription was under the line set by WHO,average numbers of antibiotic drugs per prescription and injections per prescription were over the line set by WHO,average amount per prescription of medical department was the most. Conclusion prescription evaluation program has great operability,flexibility and practicability,and could monitor the prescribing dynamically.The indicator system of the program is coincidence with the regular of drug utilization and the concept of national medical revolution policy which put much emphasis on caring the popular.
Objective To conclude the Practice and experience of prescription evaluation program. Methods To take a sample of 120 prescriptions every month during July 2007 to July 2009,calculate the average of each indicator of the prescription evaluation table designed by the Ministry of Health. Results average numbers of drugs per prescription was under the line set by WHO,average numbers of antibiotic drugs per prescription and injections per prescription were over the line set by WHO,average amount per prescription of medical department was the most. Conclusion prescription evaluation program has great operability,flexibility and practicability,and could monitor the prescribing dynamically.The indicator system of the program is coincidence with the regular of drug utilization and the concept of national medical revolution policy which put much emphasis on caring the popular.
2010, 28(2): 145-147.
Abstract:
Objective To investigate the utilization of TPN so as to provide some references for rational use in the clinic. Methods 145 cases treated with TPN were reviewed retrospectively and the medication indications and drug consumption were analyzed statistically. Results 145 cases received a total of 1 117 TPN.Problems detected in TPN therapy involved incompletion in basic components and the proportion of reimbursement was reasonable.The metabolic complication rate was 20.69%.The occurrence of complication was associated with the occasion of applying TPN. Conclusion Rational use of appling TPN should base on individualized prescription,so safe and effective nutritional support will be obtained.
Objective To investigate the utilization of TPN so as to provide some references for rational use in the clinic. Methods 145 cases treated with TPN were reviewed retrospectively and the medication indications and drug consumption were analyzed statistically. Results 145 cases received a total of 1 117 TPN.Problems detected in TPN therapy involved incompletion in basic components and the proportion of reimbursement was reasonable.The metabolic complication rate was 20.69%.The occurrence of complication was associated with the occasion of applying TPN. Conclusion Rational use of appling TPN should base on individualized prescription,so safe and effective nutritional support will be obtained.
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